WO2003081210A3 - Identification of kinase inhibitors - Google Patents

Identification of kinase inhibitors Download PDF

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Publication number
WO2003081210A3
WO2003081210A3 PCT/US2003/008725 US0308725W WO03081210A3 WO 2003081210 A3 WO2003081210 A3 WO 2003081210A3 US 0308725 W US0308725 W US 0308725W WO 03081210 A3 WO03081210 A3 WO 03081210A3
Authority
WO
Grant status
Application
Patent type
Prior art keywords
identification
protein kinase
inhibitors
kinase inhibitors
inactive conformation
Prior art date
Application number
PCT/US2003/008725
Other languages
French (fr)
Other versions
WO2003081210A2 (en )
Inventor
Andrew Braisted
John C Prescott
Original Assignee
Andrew Braisted
John C Prescott
Sunesis Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date

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Classifications

    • CCHEMISTRY; METALLURGY
    • C40COMBINATORIAL CHEMISTRY
    • C40BCOMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES, IN SILICO LIBRARIES
    • C40B30/00Methods of screening libraries
    • C40B30/04Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12QMEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/48Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
    • C12Q1/485Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00Screening for compounds of potential therapeutic value

Abstract

The invention concerns the identification of protein kinase inhibitors that preferentially bind to the inactive conformation of a target protein kinase. The inhibitors are identified by locking the target protein kinase in an inactive conformation, and using a covalent tethering approach to identify inhibitors preferentially targeting the inactive conformation.
PCT/US2003/008725 2002-03-21 2003-03-20 Identification of kinase inhibitors WO2003081210A3 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
US36689202 true 2002-03-21 2002-03-21
US60/366,892 2002-03-21

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2003578895A JP2005534286A (en) 2002-03-21 2003-03-20 Identification of kinase inhibitors
CA 2478981 CA2478981A1 (en) 2002-03-21 2003-03-20 Identification of kinase inhibitors
EP20030726092 EP1579186A4 (en) 2002-03-21 2003-03-20 Identification of kinase inhibitors

Publications (2)

Publication Number Publication Date
WO2003081210A2 true WO2003081210A2 (en) 2003-10-02
WO2003081210A3 true true WO2003081210A3 (en) 2007-07-26

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/008725 WO2003081210A3 (en) 2002-03-21 2003-03-20 Identification of kinase inhibitors

Country Status (5)

Country Link
US (1) US7202033B2 (en)
EP (1) EP1579186A4 (en)
JP (1) JP2005534286A (en)
CA (1) CA2478981A1 (en)
WO (1) WO2003081210A3 (en)

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US9556426B2 (en) 2009-09-16 2017-01-31 Celgene Avilomics Research, Inc. Protein kinase conjugates and inhibitors
US9562049B2 (en) 2012-12-21 2017-02-07 Medimmune Limited Pyrrolobenzodiazepines and conjugates thereof
US9567340B2 (en) 2012-12-21 2017-02-14 Medimmune Limited Unsymmetrical pyrrolobenzodiazepines-dimers for use in the treatment of proliferative and autoimmune diseases
US10029018B2 (en) 2013-10-11 2018-07-24 Medimmune Limited Pyrrolobenzodiazepines and conjugates thereof

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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9556426B2 (en) 2009-09-16 2017-01-31 Celgene Avilomics Research, Inc. Protein kinase conjugates and inhibitors
US9562049B2 (en) 2012-12-21 2017-02-07 Medimmune Limited Pyrrolobenzodiazepines and conjugates thereof
US9567340B2 (en) 2012-12-21 2017-02-14 Medimmune Limited Unsymmetrical pyrrolobenzodiazepines-dimers for use in the treatment of proliferative and autoimmune diseases
US10029018B2 (en) 2013-10-11 2018-07-24 Medimmune Limited Pyrrolobenzodiazepines and conjugates thereof

Also Published As

Publication number Publication date Type
US7202033B2 (en) 2007-04-10 grant
WO2003081210A2 (en) 2003-10-02 application
JP2005534286A (en) 2005-11-17 application
US20030232391A1 (en) 2003-12-18 application
EP1579186A4 (en) 2008-10-08 application
EP1579186A2 (en) 2005-09-28 application
CA2478981A1 (en) 2003-10-02 application

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